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BioAssay: AID 598731

Inhibition of Salmonella Typhimurium carbonic anhydrase 1 after 15 mins by stopped flow CO2 hydration assay at pH 8.3

Two new beta-carbonic anhydrases (CAs, EC 4.2.1.1) from the bacterial pathogen Salmonella enterica serovar Typhimurium, stCA 1 and stCA 2, were characterized kinetically. The two enzymes possess appreciable activity as catalysts for the hydration of CO(2) to bicarbonate, with k(cat) of 0.79#10(6) s(-1) and 1.0#10(6) s(-1), and k(cat)/K(m) of 5.2#10(7) M(-1) s(-1) and of 8.3#10(7) M(-1) s(-1), more ..
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 Tested Compounds
 Tested Compounds
All(34)
 
 
Active(5)
 
 
Unspecified(29)
 
 
 Tested Substances
 Tested Substances
All(38)
 
 
Active(5)
 
 
Unspecified(33)
 
 
 Related BioAssays
 Related BioAssays
AID: 598731
Data Source: ChEMBL (748882)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-02-15
Modify Date: 2014-05-25

Data Table ( Complete ):           Active    All
BioActive Compounds: 5
Description:
Title: Inhibition studies with anions and small molecules of two novel beta-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium.

Abstract: Two new beta-carbonic anhydrases (CAs, EC 4.2.1.1) from the bacterial pathogen Salmonella enterica serovar Typhimurium, stCA 1 and stCA 2, were characterized kinetically. The two enzymes possess appreciable activity as catalysts for the hydration of CO(2) to bicarbonate, with k(cat) of 0.79#10(6) s(-1) and 1.0#10(6) s(-1), and k(cat)/K(m) of 5.2#10(7) M(-1) s(-1) and of 8.3#10(7) M(-1) s(-1), respectively. A large number of simple/complex inorganic anions as well as other small molecules (sulfamide, sulfamic acid, phenylboronic acid, phenylarsonic acid, dialkyldithiocarbamates) showed interesting inhibitory properties towards the two new enzymes, with several low micromolar inhibitors discovered. As many strains of S. enterica show extensive resistance to classical antibiotics, inhibition of the beta-CAs investigated here may be useful for developing lead compounds for novel types of antibacterials.
(PMID: 21570835)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Putative Target:

ChEMBL Target ID: 22226
Target Type: UNCHECKED
Pref Name: Unchecked
Confidence: Default value - Target unknown or has yet to be assigned
Relationship Type: Default value - Target has yet to be curated
Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Ki*Ki PubChem standard valueFloatμM
2Ki activity commentKi activity commentString
3Ki standard flagKi standard flagInteger
4Ki qualifierKi qualifierString
5Ki published valueKi published valueFloatmM
6Ki standard valueKi standard valueFloatnM
7Ki data validityKi data validityString
8Ki activity commentKi activity commentString
9Ki standard flagKi standard flagInteger
10Ki qualifierKi qualifierString
11Ki published valueKi published valueFloatnM
12Ki standard valueKi standard valueFloatnM
13Ki data validityKi data validityString

* Activity Concentration.

Data Table (Concise)
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